New directions for urotensin II receptor ligands
Bibliographic record
Abstract
Abstract The urotensinergic system, formed by a G protein‐coupled receptor (GPCR) termed UT and two endogenous peptide ligands Urotensin II (UII, H‐Glu‐Thr‐Pro‐Asp‐[Cys‐Phe‐Trp‐Lys‐Tyr‐Cys]‐Val‐OH) and Urotensin II‐related peptide (URP, H‐Ala‐[Cys‐Phe‐Trp‐Lys‐Tyr‐Cys]‐Val‐OH), is currently regarded as a potential key contributor to cardiovascular functions. While multiple animal studies have shown the therapeutic potential of UT ligands for the treatment of heart failure and atherosclerosis, their lack of efficacy in clinical studies points toward a greater understanding of UT pharmacology at both the molecular and cellular levels. UII and URP are cyclic peptides that share a common and strictly conserved bioactive cyclic core (‐Cys‐Phe‐Trp‐Lys‐Tyr‐Cys‐) but differ by their extracyclic N‐terminal residues. While sharing common biological activity, these two endogenous ligands appear to be functionally selective, displaying different specific effects through the selection/stabilization of particular UT active conformations. Thus, UII and URP should be regarded as two distinct actors in the control of cardiovascular functions. In this regard, more focus on URP biological effects had to be paid, while systematic evaluation of new antagonists against both endogenous ligands appears mandatory. Overall, this review offers an overview of the actual horizon of UT pharmacology, notably concerning the development of biased ligands and allosteric modulators.
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How this classification was reachedexpand
Full frame machine prediction
Teacher imitationNot calibrated prevalence, not ground truth. Human validation pending. The Gemma side is a direct model label for every work in the frame, read from the title-only record. The Codex side is a classifier learned from the 10,348 direct Codex labels and calibrated to design-weighted sample rates; fields without enough sample support carry no Codex call. Candidate is the union of the two sides; consensus is their intersection. These outputs are machine_predicted_unvalidated and are not human labels.
Distilled classifier scores by category (both heads)
| Category | Codex | Gemma |
|---|---|---|
| Metaresearch | 0.001 | 0.001 |
| Meta-epidemiology (narrow) | 0.000 | 0.000 |
| Meta-epidemiology (broad) | 0.001 | 0.000 |
| Bibliometrics | 0.001 | 0.000 |
| Science and technology studies | 0.000 | 0.000 |
| Scholarly communication | 0.001 | 0.001 |
| Open science | 0.001 | 0.001 |
| Research integrity | 0.001 | 0.002 |
| Insufficient payload (model declined to judge) | 0.006 | 0.003 |
Machine scores (provisional)
The two teacher heads of the student model, read on this work. A score orders the frame for review; it never asserts a category, and the validation status ships verbatim with every row.
Baseline scores from an immature model (maturity gate not passed, 7 training rounds). Scores rank; they never assert a category.
score_only:v0-immature-baseline · verbatim from the scoring run: score_only means the number may rank works, and no category label ships from itClassification
machine, unvalidatedMachine predicted; a candidate call from one source (direct Gemma or distilled Codex), not a consensus.
How this classification was reached, model by model and score by score, is at the end of the page under "How this classification was reached".